AR058984A1 - Derivados de ciclohexil piperazinil metanona - Google Patents

Derivados de ciclohexil piperazinil metanona

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Publication number
AR058984A1
AR058984A1 ARP070100118A ARP070100118A AR058984A1 AR 058984 A1 AR058984 A1 AR 058984A1 AR P070100118 A ARP070100118 A AR P070100118A AR P070100118 A ARP070100118 A AR P070100118A AR 058984 A1 AR058984 A1 AR 058984A1
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AR
Argentina
Prior art keywords
substituted
alkyl
halogen
halogenoalkyl
groups independently
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ARP070100118A
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English (en)
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Hoffmann La Roche
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Application filed by Hoffmann La Roche filed Critical Hoffmann La Roche
Publication of AR058984A1 publication Critical patent/AR058984A1/es

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    • C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/16—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms
    • C07D295/18—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms by radicals derived from carboxylic acids, or sulfur or nitrogen analogues thereof
    • C07D295/182—Radicals derived from carboxylic acids
    • C07D295/185—Radicals derived from carboxylic acids from aliphatic carboxylic acids
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    • C07D295/16—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms
    • C07D295/18—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms by radicals derived from carboxylic acids, or sulfur or nitrogen analogues thereof
    • C07D295/182—Radicals derived from carboxylic acids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/04—Anorexiants; Antiobesity agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/06—Antihyperlipidemics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
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    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04—Indoles; Hydrogenated indoles
    • C07D209/08—Indoles; Hydrogenated indoles with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to carbon atoms of the hetero ring
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    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
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    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
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    • C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/36—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
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    • C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/36—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D211/40—Oxygen atoms
    • C07D211/44—Oxygen atoms attached in position 4
    • C07D211/46—Oxygen atoms attached in position 4 having a hydrogen atom as the second substituent in position 4
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    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/72—Nitrogen atoms
    • C07D213/74—Amino or imino radicals substituted by hydrocarbon or substituted hydrocarbon radicals
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    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/84—Nitriles
    • C—CHEMISTRY; METALLURGY
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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/04—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to the ring carbon atoms
    • C07D215/08—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to the ring carbon atoms with acylated ring nitrogen atom
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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D217/00—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems
    • C07D217/02—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with only hydrogen atoms or radicals containing only carbon and hydrogen atoms, directly attached to carbon atoms of the nitrogen-containing ring; Alkylene-bis-isoquinolines
    • C07D217/04—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with only hydrogen atoms or radicals containing only carbon and hydrogen atoms, directly attached to carbon atoms of the nitrogen-containing ring; Alkylene-bis-isoquinolines with hydrocarbon or substituted hydrocarbon radicals attached to the ring nitrogen atom
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    • C07D241/02—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
    • C07D241/04—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
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    • C07D241/02—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
    • C07D241/10—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
    • C07D241/14—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
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    • C07D243/00—Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms
    • C07D243/06—Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms having the nitrogen atoms in positions 1 and 4
    • C07D243/08—Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms having the nitrogen atoms in positions 1 and 4 not condensed with other rings
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    • C07D261/00—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings
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    • C07D295/16—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms
    • C07D295/20—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms by radicals derived from carbonic acid, or sulfur or nitrogen analogues thereof
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    • C07D309/00—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings
    • C07D309/02—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
    • C07D309/08—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings having no double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D309/14—Nitrogen atoms not forming part of a nitro radical

Abstract

Los compuestos son utiles para el tratamiento y/o prevencion de enfermedades que están asociadas con la modulacion de los receptores H3. Reivindicacion 1: Los compuestos de la formula general (1) en la que s es 1 o 2; R1 se selecciona del grupo que consiste en alquilo inferior, cicloalquilo, cicloalquilalquilo inferior, cianoalquilo inferior, alquilsulfonilalquilo inferior y tetrahidropiranilo; R1a es hidrogeno o alquilo inferior; R2 se selecciona del grupo que consiste en hidrogeno, alquilo inferior, halogenoalquilo inferior, alcoxialquilo inferior y cianoalquilo inferior; R3 se selecciona del grupo que consiste en -(CH2)m-arilo, en la que m es 0, 1 o 2 y en la que el anillo arilo está no sustituido o sustituido con uno, dos o tres grupos independientemente seleccionados de entre alquilo inferior, halogeno, halogenoalquilo inferior, ciano, alcoxi inferior, alcanoilo inferior, benzoilo, carbamoilo, alquilsulfonilo inferior, halogenoalquilsulfonilo inferior, halogenoalcoxi inferior, cicloalquilalcoxi inferior e hidroxialquilo inferior, -(CH2)n-heteroarilo, en la que n es 0, 1 o 2 y en la que el anillo heteroarilo no está sustituido o sustituido con uno o dos grupos independientemente seleccionados de entre alquilo inferior, halogeno, halogenoalquilo inferior, ciano, alcoxi inferior, alcanoilo inferior, benzoilo, carbamoilo, alquilsulfonilo inferior, halogenoalquilsulfonilo inferior, halogenoalcoxi inferior, cicloalquilalcoxi inferior e hidroxialquilo inferior, indanilo, 1-oxo-indanilo, -CO-(alquilo C3-8)-, -CO-(CH2)p-arilo, en la que p es 0, 1 o 2 y en la que el anillo arilo está no sustituido o sustituido con uno, dos o tres grupos independientemente seleccionados de entre alquilo inferior, halogeno, halogenoalquilo inferior, ciano, alcoxi inferior, alcanoilo inferior, benzoilo, halogenoalcoxi inferior e hidroxialquilo inferior, -CO(CH2)q-heteroarilo, en la que q es 0, 1 o 2 y en la que el anillo heteroarilo está no sustituido o sustituido con uno o dos grupos independientemente seleccionados de entre alquilo inferior, halogeno, halogenoalquilo inferior, ciano, alcoxi inferior, alcanoilo inferior, benzoilo, halogenoalcoxi inferior e hidroxialquilo inferior, y -CO-NR4R5, o R2 y R3 junto con el átomo de nitrogeno al que están unidos forman un anillo heterocíclico de 5 o 6 miembros que está condensado con un anillo fenilo, y dicho anillo fenilo está no sustituido o sustituido con uno, dos o tres grupos independientemente seleccionados de entre alquilo inferior, alcoxi inferior y halogeno; R4 se selecciona del grupo que consiste en hidrogeno, alquilo inferior, halogenoalquilo inferior, alcoxialquilo inferior y cianoalquilo inferior; R5 se selecciona del grupo que consiste en alquilo inferior, arilo no sustituido o sustituido con uno, dos o tres grupos independientemente seleccionados de entre alquilo inferior, halogeno, halogenoalquilo inferior, ciano, alcoxi inferior, alcanoilo inferior, benzoilo, halogenoalcoxi inferior e hidroxialquilo inferior, y arilalquilo inferior en el que el anillo fenilo puede no estar sustituido o sustituido con uno o dos grupos independientemente seleccionados de entre alquilo inferior, halogeno, halogenoalquilo inferior, ciano, alcoxi inferior, alcanoilo inferior, benzoilo, halogenoalcoxi inferior e hidroxialquilo inferior; o R4 y R5 junto con el átomo de nitrogeno al que están unidos forman un anillo heterocíclico de 4, 5, 6 o 7 miembros que contiene de forma opcional otro heteroátomo seleccionado de nitrogeno, oxígeno o azufre, un grupo sulfinilo o un grupo sulfonilo, y dicho anillo heterocíclico no está sustituido o sustituido con uno, dos o tres grupos independientemente seleccionados de entre alquilo inferior, halogeno, halogenoalquilo, ciano, hidroxi, hidroxialquilo inferior, alcoxi inferior, oxo, fenilo, bencilo, piridilo y carbamoilo, o está condensado con un anillo fenilo, dicho anillo fenilo está no sustituido o sustituido con uno, dos o tres grupos independientemente seleccionados de entre alquilo inferior, alcoxi inferior y halogeno; y las sales farmacéuticamente aceptables de los mismos.
ARP070100118A 2006-01-13 2007-01-11 Derivados de ciclohexil piperazinil metanona AR058984A1 (es)

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US (2) US20070167436A1 (es)
EP (1) EP1976840A1 (es)
JP (1) JP2009523150A (es)
KR (1) KR20080085031A (es)
CN (1) CN101374825A (es)
AR (1) AR058984A1 (es)
AU (1) AU2007204426A1 (es)
BR (1) BRPI0707916A2 (es)
CA (1) CA2635719A1 (es)
CL (1) CL2010000667A1 (es)
IL (1) IL192471A0 (es)
NO (1) NO20082939L (es)
RU (1) RU2008132966A (es)
TW (1) TW200736233A (es)
WO (1) WO2007080140A1 (es)
ZA (1) ZA200805679B (es)

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ZA200805679B (en) 2009-11-25
CA2635719A1 (en) 2007-07-19
CL2010000667A1 (es) 2010-11-12
AU2007204426A1 (en) 2007-07-19
US20100120769A1 (en) 2010-05-13
KR20080085031A (ko) 2008-09-22
CN101374825A (zh) 2009-02-25
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